RO2959 Hydrochloride

RO2959 Hydrochloride Chemische Eigenschaften,Einsatz,Produktion Methoden

• Biologische Aktivität

  RO2959 hydrochloride is a potent and selective CRAC channel inhibitor with IC50 of 402 nM. It is a potent blocker of Orai1/Stim1 channel-mediated calcium storage entry (SOCE) with IC50 of 25 nM. It is also a potent inhibitor of human IL-2 production, effectively blocking T cell receptor-triggered gene expression and T cell functional pathways.

• in vitro

  RO2959 hydrochloride inhibits Orai1 and Orai3 with IC ₅₀ values of 25 nM and 530 nM, respectively. It blocks store operated calcium entry (SOCE) in activated CD4+T lymphocytes with an IC < sub> 50 value of 265 nM.
  It is a potent SOCE inhibitor that blocks an IP3-dependent current in CRAC-expressing RBL-2H3 cells and CHO cells stably expressing human Orai1 and Stim1, as well as SOCE in human primary CD4 ⁺ T cells triggered by either T cell receptor (TCR) stimulation or thapsigargin treatment. RO2959 completely inhibits cytokine production as well as T cell proliferation mediated by TCR stimulation or MLR (mixed lymphocyte reaction ).

• target

  CRAC channel 402 nM (IC 50 )

  Orai1/Stim1 channels 25 nM (IC 50 )

  IL-2

RO2959 Hydrochloride Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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